A novel indigoid anti-tuberculosis agent

  • Bioorg Med Chem Lett. 2014 Jan 1;24(1):268-70. doi: 10.1016/j.bmcl.2013.11.024.
Larry L Klein  1 ,  Valentina Petukhova  2 ,  Baojie Wan  2 ,  Yuehong Wang  2 ,  Bernard D Santasiero  3 ,  David C Lankin  4 ,  Guido F Pauli  5 ,  Scott G Franzblau  5
Affiliations
  • 1. Institute for Tuberculosis Research, College of Pharmacy, University of Illinois at Chicago, 833 S. Wood Street, Chicago 60612, USA. Electronic address: [email protected].
  • 2. Institute for Tuberculosis Research, College of Pharmacy, University of Illinois at Chicago, 833 S. Wood Street, Chicago 60612, USA.
  • 3. Center for Pharmaceutical Biotechnology, College of Pharmacy, University of Illinois at Chicago, 900 S. Ashland Ave., Chicago, IL 60607, USA.
  • 4. Department of Medicinal Chemistry, College of Pharmacy, University of Illinois at Chicago, 833 S. Wood Street, Chicago 60612, USA.
  • 5. Institute for Tuberculosis Research, College of Pharmacy, University of Illinois at Chicago, 833 S. Wood Street, Chicago 60612, USA; Department of Medicinal Chemistry, College of Pharmacy, University of Illinois at Chicago, 833 S. Wood Street, Chicago 60612, USA.
PMID: 24314672 DOI: 10.1016/j.bmcl.2013.11.024
Abstract

The structure of a novel indigoid component was characterized by X-ray crystallography. This compound exhibited excellent anti-tuberculosis activity against Mycobacterium tuberculosis H37Rv in whole Cell Culture showing a submicromolar minimum inhibitory concentration (MIC). A synthesis of this molecule was designed and carried out to produce sufficient material for further testing. The in vitro profile, structure, and first synthesis of this indigoid component is reported.

Keywords
Anti-tuberculosis; Indigoid; X-ray.